EA020479B1 - СОЕДИНЕНИЯ И КОМПОЗИЦИИ КАК ИНГИБИТОРЫ ПРОТЕИНКИНАЗЫ B-Raf - Google Patents
СОЕДИНЕНИЯ И КОМПОЗИЦИИ КАК ИНГИБИТОРЫ ПРОТЕИНКИНАЗЫ B-Raf Download PDFInfo
- Publication number
- EA020479B1 EA020479B1 EA201200323A EA201200323A EA020479B1 EA 020479 B1 EA020479 B1 EA 020479B1 EA 201200323 A EA201200323 A EA 201200323A EA 201200323 A EA201200323 A EA 201200323A EA 020479 B1 EA020479 B1 EA 020479B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- methyl
- pyrimidin
- cyclopropyl
- propan
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US23808309P | 2009-08-28 | 2009-08-28 | |
US31306110P | 2010-03-11 | 2010-03-11 | |
PCT/EP2010/062495 WO2011023773A1 (en) | 2009-08-28 | 2010-08-26 | Compounds and compositions as protein kinase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201200323A1 EA201200323A1 (ru) | 2012-09-28 |
EA020479B1 true EA020479B1 (ru) | 2014-11-28 |
Family
ID=42829939
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201200323A EA020479B1 (ru) | 2009-08-28 | 2010-08-26 | СОЕДИНЕНИЯ И КОМПОЗИЦИИ КАК ИНГИБИТОРЫ ПРОТЕИНКИНАЗЫ B-Raf |
Country Status (19)
Country | Link |
---|---|
US (3) | US8242260B2 (pl) |
EP (1) | EP2470528B1 (pl) |
JP (1) | JP5726190B2 (pl) |
KR (1) | KR101714107B1 (pl) |
CN (1) | CN102596937B (pl) |
AR (1) | AR077977A1 (pl) |
AU (1) | AU2010288455B2 (pl) |
BR (1) | BR112012004448A2 (pl) |
CA (1) | CA2771673C (pl) |
EA (1) | EA020479B1 (pl) |
ES (1) | ES2527176T3 (pl) |
IN (1) | IN2012DN00869A (pl) |
JO (1) | JO3007B1 (pl) |
MX (1) | MX2012002542A (pl) |
PL (1) | PL2470528T3 (pl) |
PT (1) | PT2470528E (pl) |
TW (1) | TWI487701B (pl) |
UY (1) | UY32859A (pl) |
WO (1) | WO2011023773A1 (pl) |
Families Citing this family (23)
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JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
MX340392B (es) | 2010-02-25 | 2016-07-06 | Dana Farber Cancer Inst Inc | Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. |
WO2013059634A1 (en) | 2011-10-20 | 2013-04-25 | The Regents Of The University Of California | Use of cdk9 inhibitors to reduce cartilage degradation |
CN108542906A (zh) | 2011-11-11 | 2018-09-18 | 诺华股份有限公司 | 治疗增生性疾病的方法 |
SI2782557T1 (sl) | 2011-11-23 | 2019-02-28 | Array Biopharma, Inc., | Farmacevtske formulacije |
US9408885B2 (en) | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
US20150232452A1 (en) * | 2012-09-19 | 2015-08-20 | Ruga Corporation | Novel raf kinase inhibitors |
US9242969B2 (en) * | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
CN105228983A (zh) | 2013-05-30 | 2016-01-06 | 普莱希科公司 | 用于激酶调节的化合物及其适应症 |
MX2015016771A (es) | 2013-06-25 | 2016-03-31 | Squibb Bristol Myers Co | Compuestos de carbazol carboxamida utiles como inhibidores de cinasa. |
UY35625A (es) | 2013-06-25 | 2014-12-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos como inhibidores de quinasa |
KR20160067841A (ko) * | 2013-08-28 | 2016-06-14 | 메디베이션 테크놀로지즈, 인크. | 헤테로사이클릭 화합물 및 사용 방법 |
GB2517988A (en) * | 2013-09-09 | 2015-03-11 | Redx Pharma Ltd | Compounds |
UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
JP6930913B2 (ja) | 2014-10-14 | 2021-09-01 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアThe Regents Of The University Of California | 炎症を阻害するためのcdk9及びbrd4阻害剤の使用法 |
CN104402920B (zh) * | 2014-11-27 | 2018-04-03 | 河南科技学院 | 一种合成2‑卤代‑3‑频那醇硼酸酯‑5‑氯苯胺的方法 |
AU2017329090B9 (en) | 2016-09-19 | 2019-09-05 | Novartis Ag | Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor |
JP7341060B2 (ja) | 2017-02-10 | 2023-09-08 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | Mapk経路の活性化に関連付けられる癌の処置のための方法及び医薬組成物 |
JP7309614B2 (ja) | 2017-05-02 | 2023-07-18 | ノバルティス アーゲー | 組み合わせ療法 |
EP3732285A1 (en) | 2017-12-28 | 2020-11-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
WO2020124397A1 (en) * | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
WO2022036176A1 (en) * | 2020-08-13 | 2022-02-17 | Albert Einstein College Of Medicine | N-cyclyl-sulfonamides useful for inhibiting raf |
WO2023240024A1 (en) | 2022-06-08 | 2023-12-14 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009115572A2 (en) * | 2008-03-21 | 2009-09-24 | Novartis Ag | Novel heterocyclic compounds and uses therof |
WO2009137391A2 (en) * | 2008-05-06 | 2009-11-12 | Smithkline Beecham Corporation | Benzene sulfonamide thiazole and oxazole compounds |
WO2010010154A1 (en) * | 2008-07-24 | 2010-01-28 | Nerviano Medical Sciences S.R.L. | 3,4-diarylpyrazoles as protein kinase inhibitors |
Family Cites Families (22)
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US2659739A (en) | 1950-04-14 | 1953-11-17 | Eastman Kodak Co | 1-hydroxy-4-beta-cyanopropylamino-anthraquinone and process for preparing same |
US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
US6391636B1 (en) | 1994-05-31 | 2002-05-21 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
US6037136A (en) | 1994-10-24 | 2000-03-14 | Cold Spring Harbor Laboratory | Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto |
US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
GB2306108A (en) * | 1995-10-13 | 1997-04-30 | Merck & Co Inc | Treatment of Raf-mediated cancers with imidazole derivatives |
JP2000511419A (ja) | 1996-05-23 | 2000-09-05 | アプライド・リサーチ・システムズ・エイアールエス・ホールディング・ナムローゼ・フェンノートシャップ | Raf―1または14―3―3タンパク質のIL―2受容体β鎖への結合を阻害する化合物およびそれを含有する医薬組成物 |
AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
US6187799B1 (en) | 1997-05-23 | 2001-02-13 | Onyx Pharmaceuticals | Inhibition of raf kinase activity using aryl ureas |
GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
US6204467B1 (en) | 1998-03-24 | 2001-03-20 | Ford Global Technologies, Inc. | Method and apparatus for resistive welding |
ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
AU2001285349A1 (en) | 2000-08-30 | 2002-03-13 | The Board Of Trustees Of The University Of Arkansas | Induction of ldl receptor expression by extracellular-signal regulated kinase, erk-1/2 |
SI2130537T1 (sl) | 2002-03-13 | 2013-01-31 | Array Biopharma, Inc. | N3-alkilirani derivati benzimidazola kot inhibitorji mek |
US6644516B1 (en) | 2002-11-06 | 2003-11-11 | Continental Afa Dispensing Company | Foaming liquid dispenser |
CA2599320A1 (en) | 2005-02-25 | 2006-08-31 | Kudos Pharmaceuticals Limited | Hydrazinomethyl, hydr zonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents |
JP2008531538A (ja) | 2005-02-25 | 2008-08-14 | クドス ファーマシューティカルズ リミテッド | 2,4−ジアミノ−ピリドピリミジン誘導体とmTOR阻害剤としてのその使用 |
WO2007060404A1 (en) | 2005-11-22 | 2007-05-31 | Kudos Pharmaceuticals Limited | PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS |
AU2007204208A1 (en) | 2006-01-11 | 2007-07-19 | Astrazeneca Ab | Morpholino pyrimidine derivatives and their use in therapy |
HUE033894T2 (en) | 2006-08-23 | 2018-01-29 | Kudos Pharm Ltd | 2-Methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as MTOR inhibitors |
TW200922582A (en) | 2007-08-20 | 2009-06-01 | Organon Nv | N-benzyl, N'-arylcarbonylpiperazine derivatives |
-
2010
- 2010-08-24 US US12/862,418 patent/US8242260B2/en not_active Expired - Fee Related
- 2010-08-26 EP EP10745280.7A patent/EP2470528B1/en active Active
- 2010-08-26 KR KR1020127007838A patent/KR101714107B1/ko active IP Right Grant
- 2010-08-26 MX MX2012002542A patent/MX2012002542A/es active IP Right Grant
- 2010-08-26 PL PL10745280T patent/PL2470528T3/pl unknown
- 2010-08-26 CA CA2771673A patent/CA2771673C/en not_active Expired - Fee Related
- 2010-08-26 CN CN201080038235.XA patent/CN102596937B/zh active Active
- 2010-08-26 BR BR112012004448A patent/BR112012004448A2/pt not_active Application Discontinuation
- 2010-08-26 IN IN869DEN2012 patent/IN2012DN00869A/en unknown
- 2010-08-26 AR ARP100103125A patent/AR077977A1/es unknown
- 2010-08-26 EA EA201200323A patent/EA020479B1/ru not_active IP Right Cessation
- 2010-08-26 ES ES10745280.7T patent/ES2527176T3/es active Active
- 2010-08-26 PT PT107452807T patent/PT2470528E/pt unknown
- 2010-08-26 JO JOP/2010/0298A patent/JO3007B1/ar active
- 2010-08-26 AU AU2010288455A patent/AU2010288455B2/en not_active Ceased
- 2010-08-26 WO PCT/EP2010/062495 patent/WO2011023773A1/en active Application Filing
- 2010-08-26 JP JP2012526067A patent/JP5726190B2/ja active Active
- 2010-08-27 UY UY0001032859A patent/UY32859A/es not_active Application Discontinuation
- 2010-08-27 TW TW099128938A patent/TWI487701B/zh not_active IP Right Cessation
-
2012
- 2012-05-16 US US13/473,230 patent/US8563553B2/en active Active
-
2013
- 2013-09-10 US US14/022,540 patent/US8859548B2/en active Active
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009115572A2 (en) * | 2008-03-21 | 2009-09-24 | Novartis Ag | Novel heterocyclic compounds and uses therof |
WO2009137391A2 (en) * | 2008-05-06 | 2009-11-12 | Smithkline Beecham Corporation | Benzene sulfonamide thiazole and oxazole compounds |
WO2010010154A1 (en) * | 2008-07-24 | 2010-01-28 | Nerviano Medical Sciences S.R.L. | 3,4-diarylpyrazoles as protein kinase inhibitors |
Non-Patent Citations (1)
Title |
---|
WOLIN R.L. ET AL.: "Dual binding site inhibitors of B-RAF kinase" BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB LNKD- DOI:10.1016/J.BMCL.2008.04.002, vol. 18, no. 9, 1 May 2008 (2008-05-01), pages 2825-2829, XP022634962 ISSN: 0960-894X [retrieved on 2008-04-04] page 2827; table 1; compounds 14-16 * |
Also Published As
Publication number | Publication date |
---|---|
WO2011023773A1 (en) | 2011-03-03 |
TWI487701B (zh) | 2015-06-11 |
EP2470528B1 (en) | 2014-10-01 |
ES2527176T3 (es) | 2015-01-21 |
CN102596937B (zh) | 2014-02-12 |
TW201111365A (en) | 2011-04-01 |
JO3007B1 (ar) | 2016-09-05 |
JP2013503139A (ja) | 2013-01-31 |
AU2010288455B2 (en) | 2013-01-31 |
CA2771673C (en) | 2016-07-12 |
US8242260B2 (en) | 2012-08-14 |
KR101714107B1 (ko) | 2017-03-08 |
KR20120092577A (ko) | 2012-08-21 |
BR112012004448A2 (pt) | 2017-05-30 |
AU2010288455A1 (en) | 2012-02-23 |
EA201200323A1 (ru) | 2012-09-28 |
UY32859A (es) | 2011-03-31 |
CA2771673A1 (en) | 2011-03-03 |
US8859548B2 (en) | 2014-10-14 |
US8563553B2 (en) | 2013-10-22 |
US20110052578A1 (en) | 2011-03-03 |
EP2470528A1 (en) | 2012-07-04 |
IN2012DN00869A (pl) | 2015-07-10 |
US20120225899A1 (en) | 2012-09-06 |
MX2012002542A (es) | 2012-04-02 |
CN102596937A (zh) | 2012-07-18 |
JP5726190B2 (ja) | 2015-05-27 |
PL2470528T3 (pl) | 2015-03-31 |
AR077977A1 (es) | 2011-10-05 |
US20140011825A1 (en) | 2014-01-09 |
PT2470528E (pt) | 2014-12-29 |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |